2B : DIURETICS - CARBONIC ANHYDRASE INHIBITORS Flashcards

1
Q

Carbonic
Anhydrase Inhibitors
prototype

A

Acetazolamide

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2
Q

is an enzyme that helps
secrete cerebrospinal fluid and aqueous humor

A

Carbonic anhydrase

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3
Q

MECHANISM OF ACTION OF CARBONIC ANHYDRASE INHIBITORS

A

Inhibits carbonic anhydrase
in brush border & cytoplasm

Block NaHCO3 reabsorption
in PCT

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4
Q

Where is the action of carbonic anhydrase inhibitor

A

acts predominantly in PCT

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5
Q

use of carbonic anhydrase inhibitor

A
  1. In glaucoma,
    **secretion of aqueous humor is
    reduced **
  2. in motion sickness, metabolic acidosis increases respiration
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6
Q

Major Renal effect of
Acetazolamide

A
  1. **BICARBONATE DIURESIS
    **
    body bicarbonate
    depletion metabolic acidosis
  2. As increased Na+ reaches CCT
    excess Na+ is reabsorbed & K+ is secreted (**significant K+
    wasting )
  3. Self limiting (2 3d)
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7
Q

Acetazolamide as a Diuretic (use)

A
  1. Edema
  2. Cases resistant to diuretic
    monotherapy
    - combined with diuretics that block Na+ reabsorption at DCT marked natriuresis

Note: Long term use can lead to metabolic acidosis

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8
Q

why is acetazolmaide not widely used in treatment of edema

A

low efficacy as a single agent

used for diuretic effect only if edema is accompanied by
significant* metabolic alkalosis
*

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9
Q

Therapeutic uses of CARBONIC ANHYDRASE

A
  1. Open Angle Glaucoma
  2. to correct Metabolic Alkalosis

Major clinical applications : on carbonic anhydrase dependent HCO3‾/fluid transport at** extrarenal sites**

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10
Q

major indication OF CARBONIC ANHYDRASE

A

Open Angle Glaucoma

to lower
IOP (INTRAOCULAR PRESSURE)

  • orally, parenterally , topical (dorzolamide brinzolamide)
  • undetectable plasma levels
  • no diuretic / systemic metabolic effects
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11
Q

ADVERSE EFFECTS of carbonic anhydrase

A
  1. Hyperchloremic Metabolic Acidosis
  2. Calculus formation,
    ureteral colic
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12
Q
  • resulting from chronic HCO3 depletion
  • persists as long as CAI (carbonic anhydrase inhibitor) is continued
  • These agent cause acidosis since they force HCO3 out of the urine and so lose of bases leading to acidosis
A

Hyperchloremic Metabolic** Acidosis**

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13
Q

urine
alkalinization may cause

A

Ca2+ salt precipitation and STONE FORMATION

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14
Q

Carbonic Anhydrase Inhibitor can cause
what electrolytes in the urine

A

phosphaturia & hypercalciuria

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15
Q

Adverse Effects of
Acetazolamide

A

Sulfonamides may cause
bone marrow depression, skin toxicity,** renal lesions, hypersensitivity**

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16
Q

adverse effect of acetazolmaide in Large doses

A

drowsiness, paresthesias , renal calcium stones

17
Q

a problem with any PCT diuretic

A

Renal K+ wasting

18
Q

how to avoid renal K wasting in HF patient taking acetazolamide

A

use adenosine A1 receptor antagonists

19
Q

Carbonic Anhydrase Inhibitor in PCT act in what part of kidney

A

PCT
proximal convoluted tubule

20
Q

Uses:

A

Glaucoma,Mountain Sickness,
Eddema with alkalosis

21
Q

Side effects: Drowsiness,

A

Side effects: Drowsiness,
parestheisa , renal calcium stones, hyperchloremic metabolic acidosis,** hepatic enceph**

22
Q

Diuresis is self
limiting after

A

2-3 days